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7618650 |
Combination of a hypnotic agent and substituted bis aryl and heteroaryl compound and therapeutic application thereof
The invention concerns the combination of a short-acting hypnotic agent and a compound of formula (I):
Wherein X, Y, Z, A, B, D, Ar, R 1 and R 2 are as defined herein. The combination of this...
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7612089 |
Tetrahydroisoquinolines as factor Xa inhibitors
The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The...
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7598265 |
Compositions and methods for treating CNS disorders
The invention generally relates to thienopyridinone 5-HT 4 receptor modulators, and in particular the use of these compounds and their pharmaceutical compositions, e.g., in the treatment,...
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7592353 |
Substituted 3-amino-thieno[2,3-b]pyridine-2-carboxylic acid amide compounds and processes for preparing and their uses
Disclosed are compounds of formula (I):
wherein R 1 and R 4 are defined herein, which are useful as inhibitors of the kinase activity of the IκB kinase (IKK) complex. The compounds are...
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7592352 |
Substituted thieno and furo-pyridines
This invention relates to newly identified compounds for treating and preventing tumors and cancers, and methods for treating proliferative diseases associated with the imbalance or inappropriate...
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7576072 |
Heterocyclic inhibitors of MEK and methods of use thereof
Disclosed are compounds of the Formula I
and pharmaceutically acceptable salts and prodrugs thereof, wherein R 1 , R 2 , R 7 , R 8 and R 9 , W, X, Y and Z are as defined in the specification....
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7557101 |
4,5,6,7-tetrahydro-thieno[3,2-c] pyridine derivatives
The present invention relates to compounds of formula I
wherein R 1 and R 2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are...
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7553849 |
Compounds
A compound of formula (I)
wherein
R is methyl, ethyl, n-propyl, iso-propyl, n-butyl or allyl; R′ is hydrogen, C 1 -C 4 alkyl, C 1 -C 3 alkoxy; halogen, trifluoromethyl or OCH x F y , R″...
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7553848 |
Vanilloid receptor ligands and their use in treatments
bis-Bicyclic amides and derivatives thereof and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster...
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7528125 |
Water-soluble zinc ionophores, zinc chelators, and/or zinc complexes and use for treating cancer
Disclosed herein are novel zinc ionophores, zinc chelators and/or zinc complexes with enhanced aqueous solubility. Methods of treating cancer using at least one zinc ionophore and/or zinc chelator...
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7521460 |
Thienopyridone derivatives as kinase inhibitors
A series of thieno[2,3-b]pyridin-6(7H)-one derivatives, substituted in the 2-position by a carbonyl- or sulfonyl-linked pyrrolidin-1-yl or related moiety, being inhibitors of p38 MAP kinase, are...
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7491733 |
Bicyclic guanidine derivatives and therapeutic uses thereof
The invention relates to compounds of general formula (I), in which A, X, Y and R1 are defined in Claim 1 . These compounds may be used in the treatment of pathologies associated with insulin...
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7470707 |
Crystalline monohydrate clopidogrel naphthalenedisulfonate and process of preparation
A crystalline clopidogrel naphthalenesulfonate or a hydrate thereof, a method for preparing same, and a pharmaceutical composition containing same are provided.
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7456192 |
3β-amino azabicyclooctane heteroaromatic amid derivatives preparation method and therapeutic uses thereof
The invention concerns compounds of general formula 1, wherein: A, B, D and E represent one or two nitrogen atoms, the others being carbon atoms; X represents a S or, a O, thereby forming a...
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7449472 |
Methods of inhibiting p38 with substituted bicyclic pyrimidines
The present invention discloses compounds corresponding to the formula
wherein A, X, Y, R, R 1 and R 2 are as defined within, pharmaceutical formulations, methods of making and uses thereof.
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7439247 |
Bicyclic pyridine and pyrimidine P38 kinase inhibitors
The present invention discloses compounds corresponding to formula
wherein A, R, X, Y, R, R 1 and R 2 are as defined above, pharmaceutical formulations, methods of making and uses thereof.
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7435819 |
4,5,6,7-tetrahydro-[1,2]dithiolo[4,3-C] pyridine-3-thione compounds
The present invention relates to new compounds directly increasing kinase activity of p90 ribosomal S6 kinase 1 (RSK1), a pharmaceutical composition comprising them as active ingredient, a use...
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7425562 |
Inhibitors of cruzipain and other cysteine proteases
Compounds of general formula (I) or general formula (II)
wherein R 1 , P 1 , P 2 , Q, Y, (X) o , (W) n , (V) m , Z and U are as defined in the specification, are inhibitors of cruzipain and...
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7423047 |
Arylamine substituted bicyclic heteroaromatic compounds as p38 kinase inhibitors
Bicyclic heteroaromatic derivatives of formula (1) are described: F (1) where: the dashed line joining A and C(R a ) is present and represents a bond and A is a —N═ atom or a —C(R b )═...
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7411066 |
Amino methylated 2-pyridinones
Novel amino methylated 2-pyridinones, precursors, intermediates, and derivatives; the methods for the preparation of the same; uses of the same for inhibiting pili formation in bacteria; and...
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7407972 |
Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
The present invention provides compounds of Formula (I):
wherein A, B, C, G, and W 1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are...
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7407966 |
Thienopyridinone compounds and methods of treatment
The invention relates to 5-HT 4 receptor agonists and partial agonists. Thienopyridinone compounds and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT 4 ...
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7405226 |
Cycloalkyl-hydroxyl compounds and compositions for cholesterol management and related uses
The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions...
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7405225 |
Substituted 3-amino-thieno[2,3-b]pyridine-2-carboxylic acid amide compounds and processes for preparing and their uses
Disclosed are compounds of formula (I):
wherein R 1 and R 2 are defined herein, which are useful as inhibitors of the kinase activity of the IκB kinase (IKK) complex. The compounds are...
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7399770 |
Thieno-imino acid derivatives for use as matrix metalloproteinase inhibitors
The invention is directed to a compound of the formula I
wherein the variables are as defined herein, or
a stereoisomeric form thereof, mixture of stereoisomeric forms, in any ratio, or a...
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7381734 |
Serine protease inhibitors
Compounds of formula (I)
where R 5 , R 6a , each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.
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7371760 |
***WITHDRAWN PATENT AS PER THE LATEST USPTO WITHDRAWN LIST***
Medicinal compositions containing aspirin
A combination of 2-acetoxy-5-(α-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-
tetrahydrothieno[3,2-c]pyridine or a pharmaceutically acceptable salt thereof, and aspirin, which possess excellent...
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7371752 |
Aryl fused substituted 4-oxy-pyridines
Disclosed are compounds of the formula:
wherein X, Q, W and
are as defined herein. These compounds are agonists, antagonists or inverse agonists for GABA A brain receptors or prodrugs of...
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7365080 |
Pharmaceutical compositions comprising thieno[2,3-c]pyridine derivatives and use thereof
The present invention provides thieno[2,3-C]pyridine derivatives, pharmaceutical compositions comprising the thieno[2,3-C]pyridine derivatives, and methods of use thereof. The compounds capable of...
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7342014 |
Diamine derivatives
A compound represented by the general formula (1):
Q 1 -Q 2 -T 0 -N(R 1 )-Q 3 -N(R 2 )-T 1 -Q 4 (1)
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7332504 |
Heterocyclic substituted aminoazacycles useful as central nervous system agents
Heterocyclic substituted aminoazacyclic compounds of formula I
Z-R 3 I,
...
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7323494 |
Compounds and methods
Disclosed is a compound of having the formula:
pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables...
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7312218 |
Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors
The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula Ia-If:
or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic...
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7291639 |
Aryloxy-acetic acid compounds useful as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
This invention provides methods of inhibiting plasminogen activator inhibitor-1 (PAI-1) in a mammal, utilizing compounds of the formula:
wherein: A is C or N; B is O, S, N, or CH═CH;
...
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7285562 |
Cyanoamide compounds useful as malonyl-CoA decarboxylase inhibitors
The present invention provides methods for the use of compounds as depicted by structure I, pharmaceutical compositions containing the same, and methods for the prophylaxis, management and...
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7276519 |
Thieno[3,2-b]pyridine-6-carbonitriles and thieno[2,3-b]pyridine-5-carbonitriles as protein kinase inhibitors
This invention provides compounds of Formula (1 a )–(1 f ), II
wherein:
X, m, n, q, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , Y, Q, Z, Z′, Z′″, Z″ and J are defined...
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7276518 |
Substituted cyclohexane-1,4-diamine compounds
Substituted cyclohexane-1,4-diamine compounds, methods for production thereof, pharmaceutical compositions comprising these compounds and methods of treatment using these compounds.
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7276491 |
Anticoagulant and fibrinolytic therapy using p38 MAP kinase inhibitors
Disclosed are methods for a treating a disease or condition relating to blood coagulation and fibrinolysis using p38 MAP kinase inhibitors.
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7273876 |
Substituted bicylic thiophene derivatives, compositions containing such compounds and methods of use
The present invention addresses substituted thiophene derivatives, as well as compositions containing such compounds and methods of treatment. The compounds in the present invention are glucagon...
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7273865 |
Thiazolopyridine
The present invention relates to compounds of formula I
wherein R 1 and R 2 are described hereinbelow. These compounds have high affinity to A 2A receptors and good selectivity to A 1 and A...
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7265128 |
3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and...
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7265115 |
Diazabicyclic CNS active agents
Compounds of formula I:
or pharmaceutically acceptable salts thereof, are useful for controlling synaptic transmission in mammals.
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7253154 |
Substituted thiazolopyrimidines as xanthine oxidase inhibitors
The invention relates to compounds of the following formula (I) or their salts:
in which R 1 represents OR 4 or others, in which R 4 is an alkyl group having 1-8 carbon atoms which may have...
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7241745 |
Pyridyl alkene and pyridyl alkine acid amides as cytostatics and immunosupressives
The invention relates to a new pyridyl alkene and pyridyl alkine acid amides according to the general formula (I)
as well as methods for their production, medicaments containing these compounds...
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7208500 |
Thienopyridine-phenylacetamides and their derivatives useful as new anti-angiogenic agents
The invention relates to compounds represented by Formula (I):
and to prodrugs thereof, pharmaceutically acceptable salts or solvates of said compounds or said prodrugs, wherein each of X 1...
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7199119 |
Antiinflammation agents
Compounds, compositions and methods that are useful in the treatment of inflammatory, immunoregulatory, metabolic, infectious and cell proliferative diseases or conditions are provided herein. In...
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7192968 |
Ethylenediamine derivatives
The invention relates a compound represented by the formula (1):
Q 1 -Q 2 -C(═O)—N(R 1 )-Q 3 -N(R 2 )-T 1 -Q 4 ( 1...
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7176215 |
Bicyclic oxopyridine and oxopyrimidine derivatives
Compounds of formulae (1a) and (1b) are described: in which the dashed line represents an optional bond; A is a —N═ atom or a —N(R b )—, —C(R b )═ or —C(R b )(R C )— group; R a , R...
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7160877 |
Aliphatic nitrogen-containing 5-membered ring compound
The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]:
wherein A represents —CH 2 — or —S—, R 1 represents...
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7141564 |
Nitrogen-containing bicyclic heterocycles for use as antibacterials
Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.
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